USPTO Patents Application 09993647

• *

1VW03
4ty/ I

IN THE UNITED STATES PATENT AND TRADEMARK OFFICE

Vp

In re application of:

Bernd RIEDL et al.

Serial No.: TO BE ASSIGNED

Filed: November 27, 2001

ON

vo ~~ .

Group Art Unit: TO BE ASSIGNED
Examiner: TO BE ASSIGNED

For: gj-CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF
KINASE INHIBITORS

INFORMATION DISCLOSURE STATEMENT

Assistant Commissioner for Patents
Washington, D.C. 20231

Sir:

Copies of the references listed on the attached 1449 forms can be found in the file for
application Serial No. 09/722,418, filed November 28, 2000, which was converted to a
provisional application on November 27, 2001. Copies of these documents will be hand
carried to the Examiner if necessary for consideration of these references. The Examiner is
encouraged to contact the undersigned if any copies are needed.

Respectfully submitted,

I J. Traverso (Reg. No. 30,595)
Attorneys for Applicants

MTLLEN, WHITE, ZELANO & BRANEGAN, P.C.

Arlington Courthouse Plaza I

2200 Clarendon Boulevard, Suite 1400

Arlington, Virginia 22201

Direct Dial: (703) 812-5310

E-mail address: traverso@mwzb.com

Filed: November 27. 2001

RJT/lvb

K:\Bayer\l 8 A\ids 1 1 -27-0 1 . wpd

BAYER 18A

Form PTO-1449

U.S. DEPARTMENT OF COMMERCE
PATENT AND TRADEMARK OFFICE

INFORMATION DISCLOSURE STATEMENT
BY APPLICANT

(Use several sheets if necessary)

ATTY. DKT. NO.

SERIAL NO.

BAYER 18A

TO BE ASMCjJNED

APPLICANT

Bernd RffiDL

FILING DATE

GROUP

November 27,
2001

TO BE ASSIGNED

U.S. PATENT DOCUMENTS

Examiner
Initial

Document
Number

Date

Name

Class

Subclass

Filing Date

A A

AA

3,823,161

01109114

Lesser

A15

5,130,331

07/14/92

Pascual

H ssssss
"■■>. =

AC

4,808,588

02/28/89

King

ui*^> ■ =

A T"\

AJJ

3,424,760

01/28/69

Helsley et al.

ul < — > ==

AH/

3,424,761

01/28/69

Helsley et al.

^*J\ , z

-t -

A TJ"

Ar

3,424,762

01/28/69

Helsley et al.

oo

ACr

4,071,524

01/31/78

Banitt

A TT

AH

4,111,683

09/05/78

Singer

A T

Al

4,437,878

03/20/78

Acker et al.

AJ

4,643,849

02/17/87

Hirai et al.

a ¥y

AK

5,773,459

06/30/98

Tang et al.

A ¥

AL

5,508,288

04/16/96

Forbes et al.

AM

4,062,861

12/13/77

Yukinaga et al.

A XT

4,111,680

09/05/78

Yukinaga et al.

A /~V

AO

4,116,671

09/26/78

Yukinaga et al.

A I>

4,212,981

07/15/80

Yukinaga et al.

Ay

5,162,360

11/10/92

Creswell et al.

AR

4,514,571

04/30/85

Nakai et al.

AS

3,754,887

08/28/73

Brantley

AT

3,646,059

02/29/72

Brantley

AU

5,696,138

12/9/97

Olesen et al.

AV

5,780,483

7/14/98

Widdowson et al.

AW

4,405,644

9/20/83

Kabbe et al.

AX

4,473,579

9/25/84

Devries et al.

AY

4,526,997

7/2/85

O'Doherty et al.

AZ

4,468,380

8/28/84

O'Doherty et al.

BA

4,623,662

11/18/86

De Vries

BB

4,985,449

1/15/91

Haga et al.

BC

5,312,820

5/17/94

Ashton et al.

BD

4,410,697

10/18/83

Torok et al.

BE

4,001,256

1/4/97

Callahan et al.

BF

5,399,566

3/21/95

Katano et al.

BG

5,500,424

3/19/96

Nagamine et al.

i ♦

Sheet 2 of 5

BH

5,597,719

1/28/97

Freed et al.

BI

4,183,854

1/80 '

Crossley

BJ

3,828,001

8/74

Broad et al.

BK

4,740,520

4/88

Hallenbach et al.

BL

5,319,099

6/7/94

Kamata et al.

FOREIGN PATENT DOCUMENTS

Examiner
Initial

Document
Number

Date

Country

Class

Subclass

Translation

No

BM

EP
335156 .

Uj/ 1 1/07

IZ/LuOpCtlll

Y
A

BN

EP
459887

05/28/91

European

Y
A

x>v/

EP

371876

11/28/89

European

X

BP

C\ 1 /I A A C O

93/24458

12/9/93

WO

X

2,146,707

10/12/95

Canada

X I

BR

96/40673

12/19/96

11 T/~~\

WO

X

BS

94/14801

07/07/94

WO

X

BT

94/25012

11/10/94

wo

Y

A

BU

i con »7n

UO/ lu/Ol

X

BV

93/18028

09/16/93

WO

X

BW

94/18170

08/18/94

wo

X

BX

DE

^nSR^fi A 1
jjUjoDO r\l

02/19/83

Germany

X

BY

yj/uzjy i

ui/zo/yj

wo

VV w

Y

A

BZ

qs/1 if\&i
yj/ louo /

WO

Y

A

CA

wo

A

CB

wo

A

CC

96/40675

iz/ iy/yo

wo

A

CD

JP53
086033

7/29/78

Japan

CE

JP51

063170

1/6/76

Japan

CF

97/49400

12/31/97

WO

CG

97/49399

12/31/97

WO

CH

96/40673

12/19/96

WO

CI

99/00357

1/7/99

WO

CJ

97/45400

12/4/97

WO

CK

96/02112

3/8/90

WO

CL

99/00370

1/7/99

WO

CM

97/29743

8/21/97

WO

CN

98/22432

5/28/98

WO

CO

96/25157
Al

8/22/96

WO

CP

97/40028
Al

10/30/97

WO

Sheet 3 of 5

OTHER DOCUMENTS (Including Author, Title, Date, Pertinent Pages, Etc.)

CO

Dumas, J., "CAS Substructure," May 6, 1997, pages 1-29.

CR

Scott, Bill, "Substructure (Patent Families)," August 1 1, 1997, pages 1-19.

cs

Scott, Bill, "Substructure #2," November 25, 1997, pages 1-3.

CT

"Beilstein number" Collection, 28 pages.

CU

"Beilstein Collection," 4 pages.

CV

Scott, Bill, "Substructure Search," December 2, 1997, pages 1-51.

CX

Substructure Search, pages 1-30.

CY

Derwent World Patents Index Search, pages 20-26.

CZ

Abstract of EP 116,932

DA

Abstract of EP 676,395

TITO

A Upfront A f PIP OCY1 ^^52

DC

Abstract of EP 16,371

DD

Avruch et al., "Raf meets Ras: completing the framework of a signal transduction
pathway", TIBS 19; July 1994; pp. 279-2823.

DE

White, A. D., et al., "Heterocyclic Ureas: Inhibitors of Acyl-Co A: Cholesterol O-
Acyltransferase as Hypochelesterolemic Agents," June 6, 1996, pages 4382-95.

DF

Audia, James E., et al., "Potent, Selective Tetraphdro-B-carboline Antagonists of the
Serotonin 2B (5HT 2B ) Contractile Receptor in the Rat Stomach Fundus"' January 22, 1996,

_„ „_ Oft

pages Li /j-ou.

DG

Forbes, Ian T. , "N-( 1 -Methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: A Novel, High-
Affinity 5-HT 2B Receptor Antagonist," March 17, 1995, pages 855-57.

DH

Boulton, A. J., et al., "Heterocyclic Rearrangements. Part X. 1 A Generalised Monocyclic
Rearrangement," 1967, 2005-07.

DI

N. S. Magnuson, et al., 'The Raf-1 serine/threonine protein kinase," Cancer Biology, vol. 5,
1994, pages 247-253.

DJ

G. Daum, et al., The ins and outs of Raf Kinases,:" TIBS 19, November 1994, pages 474-
on

oU. ■

DK

W. Kolch, et al., "Raf-1 protein kinase is required for growth of induced NIH/3T3 cells,"
Letters to Nature, vol. 349, January 31, 1991, page 226-28.

DL

M. Fridman. et al., "The Minimal Fragments of c-Raf-1 and NF1 That Can Suppress v-Ha-
Ras-Induced Malignant Phenotype " The Journal of Biological Chemistry, vol. 269, no. 48,

ria^omKai. 1 lOOyT narroc 1 MS 1 lift

uecemuer z, lyy'f, pages juiuj-iuo.

DM

G. L. Bolton, et al., Chapter 17. Ras Oncogene Directed Approaches in Cancer
LJiemotnerapy, Annual ixepoirs in ivieuicindi \^nemiairy, vui. ^.v, i77t, pages iuj

DN

J. L. Bos, "ras Oncogenes in Human Cancer: A Review," Cancer Research, vol. 49,
oeptemoer i, ivoy, pages h-ooz-ov.

uu

A/firhaplic Tnctns Tiehio«Ann Phem fTT APRFI ^97 1913 143

DP

B. P. Monia, et al., "Antitumor activity of a phosphorothioate antisense
oiigodeopxynucleotide targeted against C-raT kinase," Nature Medicine, vol. 2, No. 6, June
1996, pages 668-75.

DQ

Lee, et al., Bicyclic Imidazoles as a Novel Class of Cytokine Biosynthesis Inhiibitors," N.Y.
Academy of Science, 1993, pages 149-70.

DR

F. Lepage, et al., "New N-aryl isoxazolecarboxamides and N-isoxazolybenzamides as
anticonvulsant agents," Eur. J. Med. Chem, vol. 27, 1992, pages 581-93.

DS

Ridley, et al., "Actions of JL-1 are Selectively Controlled by p38 Mitogen- Activated Protein
Kinase," The American Association of Immunologists, 1997, page 3165-73.

DT

Chemical Abstract, Vol. 116, No. 21, 25 May 1992, pages 741-742.

I

Sheet 4 of 5

U.S. PATENT DOCUMENTS

Examiner
Initial

Tlfipiimpnt

1/UtUlUvlll

Number

Date

Name

Class

Subclass

Filing Date

DU

5,059,614

10/22/91

Lepage et al.

DV

3,743,498

7/3/73

Brantley

DW

3,547,940

12/15/70

Brantley

DX

5,432,468

7/11/95

Moriyama et al.

DY

1,742,156

2/31

Fitzky

DZ

2,046,375

7/36

Goldstein et al.

EA

2,093,265

9/36

Coffby et al.

EB

2,288,422

6/42

Rohm

EC

2,683,082

7/54

Hill et al.

ED

2,745,874

5/56

Schetty et al.

EF

2,781,330

2/57

Downey

EG

2,867,659

1/59

Model et al.

EH

2,877,268

3/59

Applegate et al.

EI

2,960,488

11/60

Tamblyn et al.

EJ

3,689,550

9/72

Schellenbaum et al.

EK

3,860,645

1/95

Nikawitz

EL

5,423,905

6/95

Fringeli

EM

2,973,386

2/61

Weldon

EN

3,230,141

1/66

Frick et al.

EO

4,863,924

9/89

Haga et al.

EP

4,511,571

4/85

Bbger et al.

EQ

4,173,638

11/79

Nishiyama et al.

ER

4,173,637

11/79

Nishiyama et al.

ES

4,820,871

4/89

Kissener et al.

ET

4,983,605

1/91

Kondoet al.

EU

5,098,907

3/92

Kondoet al.

EV

5,036,072

7/91

Nakajama et al.

EW

5,470,882

11/95

Dixon et al.

EX

5,429,918

7/95

Seto et al.

EY

3,151,023

9/64

Martin

EZ

3,200,035

8/65

Martin et al.

FA

5,807,891

9/15/98

Bold et al.

FB

4,009,847

3/1/77

Aldrich et al.

FOREIGN PATENT DOCUMENTS

Examiner
Initial

Document
Number

Date

Country

Class

Subclass

Translation

Yes

No

FC

95/33458

12/14/95

wo

FD

0 771 333

3/57

Great Britain

FE

0 921 682

3/63

Great Britain

FF

0 253 997

2/88

East Germany

FG

0 405 233

1/91

Europe

4

Sheet 5 of 5

FH

1 457 172

9/66

France

FI

0 487 014

12/29

Germany

FJ

0 511 468

10/30

Germany

FK

0 523 437

5/31

Germany

FL

44 2569

2/69

Japan

FM

55 98152

7/80

Japan

FN

94 22807

10/94

WIPO

FO

3 532 47

3/91

Japan

FP

0 828 231

10/56

Great Britain

FQ

50-149668

11/75

Japan

FR

55-162772

12/80

Japan

FS

60-76072

6/75

Japan

FT

51-80862

7/76

Japan

FU

50-77375

6/75

Japan

FV

55-124763

9/80

Japan

FW

0 502 504 Al

9/92

Europe

OTHER REFERENCES (Including Author, Title, Date, Pertinent Pages, etc.)

FX

Tarzia, G. et al. "Whythesis and anti-inflammatory properties of some pyrrolo(lH3H)[3,41pyrirnidin-2-ones and
Trolo(lH,3H)r3,4-dlpyurimidin-2-ones and pyrroIo(TH,3H)-pyrimidin-2-ones. Chemical Abstracts. 27 August
79, No. 74558p; page 594.

FY

Abstract WO 9922103 , Hedge 28 May 1998

FZ

Examiner

Date Considered

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K:\Bayer\18A\1449.wpd

SHEET 1 OF 2

Form PTO 1 449 " U.S. DEPARTMENT OF COMMERCE
(Modified) PATENT AND TRADEMARK OFFICE

LIST OF REFERENCES CITED BY APPLICANT

ATTY DOCKET NO.

BAYER 18A

SERIAL NO.

TO BE ASSIGNED

APPLICANT

Bernd RIEDL et al.

FILING DATE

November 27, 2001

GROUP

TO BE ASSIGNED

U.S. PATENT DOCUMENTS

EXAMINER
INITIAL

DOCUMENT
NUMBER

DATE

NAME

C
L
A
S
S

SUB CLAab

FILING DATE
IF APPROPRIATE

AA

— —

AB

si

AC

AD

• r - ■ \
=>2>

AE

■ vo^b^;

■5t"OV - - >

AF

AG

AH

Al

AJ

AK

AL

AM

FOREIGN PATENT DOCUMENTS

DOCUMENT
NUMBER

DATE

COUNTRY

TRANSLATION
YES NO

AN

9,852,559

.11/1998

WO

AO

9,852,558

11/1998

WO

AP

9,932,436

7/1999

WO

AQ

9,932,106

7/1999

WO

AR

9,932,455

7/1999

WO

AS

9,932,463

7/1999

WO

AT

9,932,111

7/1999

WO

AU

9,932,110

4/1999

WO

AV

9,933,458

11/1998

WO

OTHER REFERENCES (Including Author, Title, Date, Pertinent Pages, etc.)

AW

Appln No. 08/863,021, May 23, 1997, RAF Kinase Inhibitors

AX

Appln No. 08/863,022, May 23, 1997, RAF Kinase Inhibitors

AY

Unassigned, December 22, 1 998, Inhibition of RAF Kinase Using Symmetrical Substituted Diphenyl Ureas

AZ

Appln No. 09/479,125, December 22, 1998, Inhibition of RAF Kinase Using Substituted Heterocyclic Ureas (Abandoned in
favor of Bayer 8C1 Serial No. 09/640,780 filed August 18, 2000)

Examiner

Date Considered

"Examiner: Initial if reference is considered, whether or not citation is in conformance with MPEP 609; Draw line through citation if not in
conformance and not considered. Include copy of this form with next communication to applicant.

K:\Bayer\18A\1449 Part 1 9-1 0-01 .wpd

Form PTO 1 449 U.S. DEPARTMENT OF COMMERCE
(Modified) PATENT AND TRADEMARK OFFICE

LIST OF REFERENCES CITED BY APPLICANT

ATTY DOCKET NO.

BAYER 18A

SERIAL NO.

TO BE ASSIGNED

APPLICANT

Bernd RIEDL et al.

FILING DATE

November 27, 2001

GROUP

TO BE ASSIGNED

OTHER REFERENCES (Including Author, Title, Date, Pertinent Pages, etc.)

AAA

Appln No. 09/472,232, December 27, 1998, Inhibition of RAF Kinase Using Aryl and Heteroaryl
Substituted Heterocyclic Ureas

AAB

Appln No. 09/458,015, December 10, 1999, Inhibition of P38 Kinase Activity Using Symmetrical and
Unsymmetrical Diphenyl Ureas

AAC

Appln No. 09/458,014, December 10, 1999, Inhibition of P38 Kinase Activity Using Substituted
Heterocyclic Ureas

AAD

Unassigned, December 22, 1998, Inhbition of RAF Kinase Using Aryl and Heteroaryl Substituted
Heterocyclic Ureas

AAE

Appln No. 09/425,229, October 22, 1999, co-Carboxy Arly Substituted Diphenyl Ureas P38 Kinase
Inhibitors

AAF

Kubo, Hiroshi et al. "Herbicidal activity of 1 ,3,4-thiadiazole derivatives" J. Agr. Food Chem. (1970) ,
18(1), 60-5

AAG

Caplus 95:61995, Abstract JP 55162772, Substituted acetic derivatives., Shionogi & Co., May 23, 1980

AAH

Caplus 86:72448, Abstract JP 57053785, Pyridine derivatives, Maeda Ryozo et al., November 15, 1982

AAI

Caplus 84:180049, Abstract JP 56029871, Hamada Yoshinori et al., July 10, 1981

AAJ

Caplus 84:43857, Abstract JP 58021626, Maeda Ryozo et al., May 2, 1983

AAK

AAL

AAM

AAN

AAO

AAP

Examiner Date

Considered

'Examiner: Initial if reference is considered, whether or not citation is in conformance with MPEP 609; Draw line through
citation if not in conformance and not considered. Include copy of this form with next communication to applicant.

K:\Bayer\1 8AM449 part 2 9-1 0-O1 .wpd

• *

SHEET 1 OF 2

Form PTO 1 449 U.S. DEPARTMENT OF COMMERCE
(Modified) PATENT AND TRADEMARK OFFICE

LIST OF REFERENCES CITED BY APPLICANT

ATTY DOCKET NO. I
BAYER 18A j

SERIAL NO.

TO BE ASSIGNED

APPLICANT

Bernd RIEDL

FILING DATE

November 27, 2001

GROUP

TO BE ASSIGNED

U.S. PATENT DOCUMENTS

EXAMINER
INITIAL

DOCUMENT
NUMBER

DATE

NAME

CLASS

OU D

CLASS

Fll ING DATE

1 11-11 iVul L-//A 1 l_

IF APPROPRIATE

AA

5,429,918

4 July. 1995

Seto ET AL.

AB

5,814,646

9/29/1998

HEINZ

AC

R/1 fi/1 Q77

HARrcn

AD

3,990,879

1 1 /9/1 976

Soper

M £J ==

^g? B

AE

5,185,358

2/09/1993

Creswell

AF

OQ ^gr

AG

•1-1 B-ss

AH

Al

AJ

AK

AL

AM

AN

FOREIGN PATENT DOCUMENTS

DOCUMENT
NUMBER

DATE

COUNTRY

TRANSLATION
YES NO

AO

16371

3/5/80

EP

AP

676395

7/17/1996

EP

AQ

2436179

2/6/1975

DE

AR

242666

10/28/1987

EP

AS

99/32111

7/01/1999

WO

AT

99/32455

7/01/1999

WO

AU

99/24398

5/20/1999

WO

AV

98/52559

11/26/1998

WO

OTHER REFERENCES (Including Author, Title, Date, Pertinent Pages, etc.)

AW

Kubo, Hiroshi et al: "herbicidal activity..." J. Agr. Food Chem, (1970), 18(1), 60-5

AX

Russo, F. et al. "Synthesis of 2,6-substituted derivatives of 5H-1 ,3,4-thiadiazolo'3,2-a!-s triazine-5,7-dione" FARMACO,
ED.SCI. (1978), 33(12), 972-83

AY

Foussard-Blanpin, Odette: "Comparative pharmacodynamic study of variously substituted carboxamides of the central
nervous ststem" Ann. Pharm. Fr. (1982), 40 (4), 339-50

AZ

Grant, A.M et al.: "Hypotensive thiadiazoles" J.Med. Chem. (1972), 15(10), 1082-4

Examiner

Date Considered

'Examiner: Initial if reference is considered, whether or not citation is in conformance with MPEP 609; Draw line through citation if not in
conformance and not considered. Include copy of this form with next communication to applicant.

JJB:K:\Bayer\18A\pg 7 of 1449 forms.wpd

SHEET 2 OF 2

FormPTO 1449
(Modified)

U.S. DEPARTMENT OF COMMERCE
PATENT AND TRADEMARK OFFICE

ATTY DOCKET NO. j
BAYER 18A J

SERIAL NO.

TO BE ASSIGNED

LIST OF REFERENCES CITED BY APPLICANT

APPLICANT

Reidl et al.

FILING DATE

November 27, 2001

GROUP

TO BE ASSIGNED

U.S. PATENT DOCUMENTS

EXAMINER
INITIAL

DOCUMENT
NUMBER

DATE

NAME

CLASS

SUB CLASS

Fll nATF
I IL.IINU Un 1 c

IF APPROPRIATE

AA

5,698,581

12/16/97

KLEEMANN ET AL.

AB

4,760,063

07/26/88

HALLENBACH ET AL

AC

I C/£0/OU

UICKORE ET AL.

AD

5,908,865

6/1/1999

DOI ET AL.

AE

6,080,763

6/27/2000

REGAN ET AL.

AF

AG

AH

Al

AJ

AK

AL

AM

AM

FOREIGN PATENT DOCUMENTS

DOCUMENT
NUMBER

DATE

COUNTRY

TRANSLATION
YES NO

AO

DE 35 29 247 A1

8/20/85

Germany

AP

DE 35 40 377 A1

11/14/85

Germany

AQ

00/17175

09/16/99

WO

AR

99/23091

5/14/1999

WO

AS

98/22103

5/28/1998

WO

AT

00/43384

7/27/2000

wo

AU

00/55152

9/21/2000

wo

AV

00/55139

9/21/2000

wo

OTHER REFERENCES (Including Author, Title, Date, Pertinent Pages, etc.)

AW

Abstract of EP 676,395 (U.S. equivalent 5,698,581)

AX

Abstract of EP 4931 (U.S. equivalent 4,240,820)

AY

Abstract of DE 3305866 (EP equivalent 1 1 6,932)

AZ

Abstract of EP 202,538

Examiner

Date Considered

"Examiner: Initial if reference is considered, whether or not citation is in conformance with MPEP 609; Draw line through citation if not in
conformance and not considered. Include copy of this form with next communication to applicant.

RJTMvb:K:\BayeA18A\pg 6 of 1449 forms.wpd